RU2016134406A - Композиции апилимода и способы их применения - Google Patents

Композиции апилимода и способы их применения Download PDF

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RU2016134406A
RU2016134406A RU2016134406A RU2016134406A RU2016134406A RU 2016134406 A RU2016134406 A RU 2016134406A RU 2016134406 A RU2016134406 A RU 2016134406A RU 2016134406 A RU2016134406 A RU 2016134406A RU 2016134406 A RU2016134406 A RU 2016134406A
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apilimod
composition
additional active
agents
cell lymphoma
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RU2016134406A
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RU2016134406A3 (ru
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Хенри ЛИХЕНШТЕЙН
Джонатан М. РОТБЕРГ
София ГЕЙЛ
Нил БИХАРРИ
Пол БЕКЕТТ
Шон ЛАНДРЕТТЕ
Крис КОНРАД
Мэтт ДАЙЕР
Тянь СЮЙ
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Лэм Терапьютикс, Инк.
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41781,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/475Quinolines; Isoquinolines having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine
    • AHUMAN NECESSITIES
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
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    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • AHUMAN NECESSITIES
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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
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    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
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  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)

Claims (23)

1. Способ лечения рака у пациента, нуждающегося в этом, включающий введение указанному пациенту терапевтически эффективного количества композиции апилимода, либо отдельно, либо в комбинации с одним или более дополнительных активных агентов.
2. Способ по п. 1, где композиция апилимода содержит свободное основание апилимода или димезилат апилимода.
3. Способ по п. 1 или 2, где композиция апилимода находится в пероральной лекарственной форме или лекарственной форме, подходящей для внутривенного введения.
4. Способ по любому из пп. 1-3, где злокачественное заболевание представляет собой лимфому, предпочтительно, В-клеточную лимфому, наиболее предпочтительно, неходжкинскую В-клеточную лимфому.
5. Способ по п. 4, где неходжкинская В-клеточная лимфома выбрана из диффузной крупноклеточной В-клеточной лимфомы (DLBCL), лимфомы Беркита, В-клеточной лимфомы средостения и лимфомы клеток мантии.
6. Способ по п. 4, где неходжкинская В-клеточная лимфома представляет собой DLBCL.
7. Способ по п. 6, где DLBCL представляет собой DLBCL-GCB.
8. Способ по любому из пп. 1-7, где способ включает введение апилимода в комбинации по меньшей мере с одним дополнительным активным агентом.
9. Способ по п. 8, где по меньшей мере один дополнительный активный агент представляет собой терапевтический агент или нетерапевтический агент, или их комбинации.
10. Способ по п. 8, где по меньшей мере один дополнительный активный агент вводят в одной лекарственной форме с композицией апилимода или в отдельных лекарственных формах с композицией апилимода.
11. Способ по п. 9 или 10, где по меньшей мере один дополнительный активный агент выбран из группы, состоящей из алкилирующего агента, интеркалирующего агента, агента, связывающего тубулин, кортикостероида и их комбинаций.
12. Способ по п. 9 или 10, где по меньшей мере один дополнительный активный агент представляет собой терапевтический агент, выбранный из группы, состоящей из ибрутиниба, ритуксимаба, доксорубицина, преднизолона, винкристина, велкада и эверолимуса, и их комбинаций.
13. Способ по п. 9 или 10, где по меньшей мере один дополнительный активный агент представляет собой терапевтический агент, выбранный из циклофосфамида, гидроксидаунорубицина (также называемого доксорубицином или Adriamycin™), винкристина (также называемого Oncovin™), преднизона, преднизолона и их комбинаций.
14. Способ по п. 9 или 10, где по меньшей мере один дополнительный активный агент представляет собой нетерапевтический агент, выбранный для облегчения одного или более побочных эффектов композиции апилимода.
15. Способ по п. 14, где нетерапевтический агент выбран из группы, состоящей из оданестрона, гранизетрона, долазетрона и палонозетрона.
16. Способ по п. 14, где нетерапевтический агент выбран из группы, состоящей из пиндолола и рисперидона.
17. Композиция апилимода для лечения рака у пациента, содержащая свободное основание апилимода или димезилат апилимода, в комбинации с одним или более из алкилирующих агентов, интеркалирующих агентов, агентов, связывающих тубулин и кортикостероидов.
18. Композиция по п. 17, где композиция содержит один или более агентов из ибрутиниба, ритуксимаба, доксорубицина, преднизолона, винкристина, велкада и эверолимуса.
19. Композиция по п. 18, где композиция содержит один или более агентов из преднизолона, велкада и эверолимуса.
20. Композиция по п. 18, где композиция содержит ибрутиниб.
21. Композиция по п. 18, где композиция содержит винкристин.
22. Композиция по любому из пп. 18-21, где композиция дополнительно содержит один или более агентов из оданестрона, гранизетрона, долазетрона, палонозетрона, пиндолола и рисперидона.
23. Способ по любому из пп. 1-16, или композиция по любому из пп. 17-22, где пациент страдает раком, который не поддается лечению или рецидивирует.
RU2016134406A 2014-01-24 2015-01-23 Композиции апилимода и способы их применения RU2016134406A (ru)

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US201461931078P 2014-01-24 2014-01-24
US201461931075P 2014-01-24 2014-01-24
US61/931,075 2014-01-24
US61/931,078 2014-01-24
US201462077127P 2014-11-07 2014-11-07
US62/077,127 2014-11-07
PCT/US2015/012733 WO2015112888A1 (en) 2014-01-24 2015-01-23 Apilimod compositions and methods for using same

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